Structure-based Drug Design and Synthesis of PARP Inhibitors: Poly(ADP-ribose)polymerase-1 Inhibitors - Softcover

Murahari, Manikanta

 
9786200437785: Structure-based Drug Design and Synthesis of PARP Inhibitors: Poly(ADP-ribose)polymerase-1 Inhibitors
Softcover
ISBN 10: 6200437785 ISBN 13: 9786200437785
Verlag: LAP LAMBERT Academic Publishing, 2019

Inhaltsangabe

Poly(ADP-ribose)polymerase (PARP) is a chromatin bound nuclear enzyme which gets activated by DNA breaks, uses NAD as substrate and catalyses the poly-ADP ribosylation of a variety of proteins. The enzyme PARP is considered as a suitable target for anti-cancer activity as it is involved in a variety of physiological functions like cellular proliferation, differentiation, apoptosis and DNA replication. Based on the literature, pharmacophoric templates and bio-isosteric replacement approach, quinazolinone and phthalazinone derivatives were selected to design molecules to calculate binding affinity and visualize binding conformations and interactions at the active pocket of target PARP-1 protein. For preliminary evaluation, in silico potential compounds were selected to synthesize, purified by column chromatography, characterized by HNMR and Mass Spectral studies and carried out for in vitro cytotoxicity. Molecular docking and preliminary experimental data helped to investigate Structure Activity Relationship for design of safe and potential PARP-1 inhibitors for cancer therapy.

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Über die Autorin bzw. den Autor

Dr. Manikanta Murahari is an academic researcher presently working as Assistant Professor at Department of Pharmaceutical Chemistry, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore. He works on hit identification for targets of Cancer, HIV & TB by Structure and Ligand based approaches using computational tools.

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Verlag
LAP LAMBERT Academic Publishing
Erscheinungsdatum
2019
Sprache
Englisch
ISBN 10 
6200437785
ISBN 13 
9786200437785
Einband
Taschenbuch
Anzahl der Seiten
108
Kontakt zum Hersteller
Nicht verfügbar
Verantwortliche Person
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